The present invention relates to antibacterial agents of the 1-carba-1-dethiaceph-3-em-4-carboxylate (Carbaceph) class in which the six membered ring of the nucleus is substituted with a thioheteroaryl group at position three.
Cephoxitin was an early cephalosporin antibacterial agent having a broad spectrum; it has the following formula: ##STR2##
The 1-carba-1-dethiaceph-3-em-4-carboxylate compounds of the present invention have activity against gram positive and gram negative microorganisms, and are useful against methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS). The antibacterial compounds of the present invention thus comprise an important contribution to therapy for these difficult to control pathogens.
Moreover, there is an increasing need for agents effective against such pathogens (MRSA/MRCNS) which are at the same time safe, i.e., relatively free from undesirable side effects.